Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
Kleinman
E F
EF
Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA.
Campbell
E
E
Giordano
L A
LA
Cohan
V L
VL
Jenkinson
T H
TH
Cheng
J B
JB
Shirley
J T
JT
Pettipher
E R
ER
Salter
E D
ED
Hibbs
T A
TA
DiCapua
F M
FM
Bordner
J
J
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D001665:Binding Sites; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D006877:Hydroxamic Acids / Q000737:chemistry*; D008956:Models, Chemical; D015394:Molecular Structure; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D011760:Pyrrolidinones / Q000737:chemistry* / Q000494:pharmacology*; D020889:Rolipram; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors*
D006877:Hydroxamic Acids; D010726:Phosphodiesterase Inhibitors; D011760:Pyrrolidinones; D014409:Tumor Necrosis Factor-alpha; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D020889:Rolipram